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固体脂质纳米粒作为干粉的开发:特性描述和配方考虑因素。

Development of Solid Lipid Nanoparticles as Dry Powder: Characterization and Formulation Considerations.

机构信息

Department of Drug and Health Science, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.

出版信息

Molecules. 2023 Feb 5;28(4):1545. doi: 10.3390/molecules28041545.

DOI:10.3390/molecules28041545
PMID:36838532
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9967033/
Abstract

Solid lipid nanoparticles (SLNs) are lipid-based colloidal systems used for the delivery of active compounds. Although SLNs have many benefits, they show important issues due to physical and chemical instability phenomena during storage. For these reasons, it is highly desirable to have a dried SLN formulation available. Therefore, the aim of the project was to identify suitable methods to obtain a dry powder formulation from an SLN suspension. The nanoparticle suspension was dried using both freeze- and spray-drying techniques. The suitability of these methods in obtaining SLN dry powders was evaluated from the analyses of nanotechnological parameters, system morphology and thermal behavior using differential scanning calorimetry. Results pointed out that both drying techniques, although at different yields, were able to produce an SLN dry powder suitable for pharmaceutical applications. Noteworthily, the freeze-drying of SLNs under optimized conditions led to a dry powder endowed with good reconstitution properties and technological parameters similar to the starting conditions. Moreover, freeze-thaw cycles were carried out as a pretest to study the protective effect of different cryoprotectants (e.g., glucose and mannitol with a concentration ranging from 1% to 10% /). Glucose proved to be the most effective in preventing particle growth during freezing, thawing, and freeze-drying processes; in particular, the optimum concentration of glucose was 1% /.

摘要

固体脂质纳米粒 (SLN) 是一种基于脂质的胶体系统,用于输送活性化合物。尽管 SLN 有许多优点,但它们在储存过程中由于物理和化学不稳定性现象而表现出重要问题。出于这些原因,非常希望有可用的干燥 SLN 制剂。因此,该项目的目的是确定从 SLN 混悬液获得干粉制剂的合适方法。使用冷冻干燥和喷雾干燥技术对纳米混悬液进行干燥。使用差示扫描量热法分析纳米技术参数、系统形态和热行为来评估这些方法获得 SLN 干粉的适用性。结果表明,尽管两种干燥技术的产率不同,但都能够生产出适用于药物应用的 SLN 干粉。值得注意的是,在优化条件下对 SLN 进行冷冻干燥会得到一种具有良好再分散性能的干粉,其技术参数与初始条件相似。此外,还进行了冻融循环作为预试验,以研究不同冷冻保护剂(例如浓度为 1% 至 10% / 的葡萄糖和甘露醇)的保护作用。葡萄糖被证明在防止冷冻、解冻和冷冻干燥过程中的颗粒生长方面最有效;特别是,葡萄糖的最佳浓度为 1% / 。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/9896bfb337d7/molecules-28-01545-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/bb1fbd0d271e/molecules-28-01545-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/3d070440538e/molecules-28-01545-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/b45e62fdcc79/molecules-28-01545-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/e64ea6bf0ce7/molecules-28-01545-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/467b682b705a/molecules-28-01545-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/580bbf6cbd30/molecules-28-01545-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/f781edf98bea/molecules-28-01545-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/9896bfb337d7/molecules-28-01545-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/bb1fbd0d271e/molecules-28-01545-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/3d070440538e/molecules-28-01545-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/b45e62fdcc79/molecules-28-01545-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/e64ea6bf0ce7/molecules-28-01545-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/467b682b705a/molecules-28-01545-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/580bbf6cbd30/molecules-28-01545-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/f781edf98bea/molecules-28-01545-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b769/9967033/9896bfb337d7/molecules-28-01545-g008.jpg

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